In vivo positron emission tomography (PET) imaging with an αvβ6 specific peptide radiolabeled using 18F-"click" chemistry:: Evaluation and comparison with the corresponding 4-[18F]fluorobenzoyl- and 2-[18F]fluoropropionyl-peptides

被引：84
作者：
Hausner, Sven H.
Marik, Jan
Gagnon, M. Karen J.
Sutcliffe, Julie L. [1 ]
机构：
[1] Univ Calif Davis, Dept Biomed Engn, Davis, CA 95616 USA
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 19期
关键词：
D O I：
10.1021/jm800608s
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Numerous radiolabeled peptides have been utilized for in vivo imaging of a variety of cell surface receptors. For applications in PET using [F-18]fluorine, peptides are radiolabeled via a prosthetic group approach. We previously developed solution-phase F-18-"click" radio-labeling and solid-phase radiolabeling using 4-[F-18]fluorobenzoic and 2-[F-18]fluoropropionic acids. Here we compare the three different radiolabeling approaches and report the effects on PET imaging and pharmacokinetics. The prosthetic groups did have an effect; metabolites with significantly different polarities were observed.
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页码：5901 / 5904
页数：4
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